PHY34是一种晚期自噬抑制剂,具有纳摩尔水平的抑制作用。在体内,PHY34具有抗高级别浆液性卵巢癌(HGSOC)活性。
产品描述
PHY34 is a late stage autophagy inhibitor with nanomolar level inhibitory effect and anti-tumor activity against high-grade serous ovarian cancer (HGSOC) in vivo.
体外活性
In HGSOC cell lines, PHY34 showed cytotoxicity with IC50 of 4 nM. Its IC50 values in MDA-MB-435 and MDAMB-231 cell lines were 23 nM and 5.2 nM, respectively. In OVCAR3 cells, 100 nM PHY34 increased the level of early and late apoptotic cells [1].
体内活性
In the hollow fiber deflector, PHY34 significantly inhibited the growth of cancer cells; In the transplanted tumor model, PHY34 reduced the ovarian tumor load. The bioavailability of mice was 56.6% after intravenous injection of 0.6 mg/kg, intraperitoneal injection of 1.8 mg/kg or oral administration of 75 mg/kg PHY34, and 2.5% after oral administration. After oral administration, the systemic clearance (CL) was 194.1 L/hr/kg, which was nearly 40 times the liver blood flow of mice, indicating that PHY34 had significant extrahepatic clearance. After oral administration, PHY34 was rapidly absorbed, and Tmax was 0.25 hr [1].
Cas No.
2130033-55-3
分子式
C30H30O12
分子量
582.55
储存和溶解度
Ethanol:10 mg/mL
DMSO:PBS (pH 7.2) (1:3):0.25 mg/mL
DMF:30 mg/mL
DMSO:90mg/mL (154.5mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years